Composition for increasing permeability of blood-brain barrier comprising nitric oxide donor and use thereof
A technology of nitric oxide and blood-brain barrier, which can be applied in the direction of active ingredients of nitro compounds, active ingredients of heterocyclic compounds, and medical preparations containing active ingredients, and can solve problems such as restrictions
Pending Publication Date: 2021-08-13
POSTECH ACAD IND FOUND
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Problems solved by technology
[0004] At the same time, a variety of drugs for the treatment of brain diseases have also been developed, but the treatment methods using existing drug systems are subject to many restrictions due to the blood-brain barrier
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[0082] Production Example: Synthesis of Nitric Oxide Donor
[0083] In order to introduce nitric oxide into the secondary amino group of pyrrolidine (Pyrrolidine), nitrogen monoxide gas was mixed with methanol (methanol), acetonitrile (acetonitrile) and ether ( diethyl ether) was used as a solvent for two days to synthesize pyrrolidine NONOate represented by chemical formula (3). Synthesis or absence of nitric oxide donors by nuclear magnetic resonance (NMR) (see figure 2 ) was confirmed, and the amount of nitric oxide released in the aqueous solution was confirmed by chemiluminescence (Chemiluminescence).
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Abstract
A composition for increasing blood-brain barrier permeability comprising a nitric oxide donor and uses thereof are included. The present invention relates to a composition to be used for increasing the blood-brain barrier permeability, the composition including a nitric oxide donor, and a use of the composition. More particularly, the invention relates to a composition to be used for increasing the blood-brain barrier permeability, the composition including a nitric oxide donor capable of carrying nitric oxide (NO), wherein the nitric oxide delivered to a site adjacent to the blood-brain barrier by the nitric oxide donor activates matrix metallopeptidase-9 (MMP-9), and the activated MMP-9 weakens a tight junction between a cerebrovascular endothelial cell and a cerebrovascular endothelial cell to increase the blood-brain barrier permeability, and to a use of the composition.
Description
technical field [0001] The present invention relates to a composition comprising a nitric oxide donor for enhancing the permeability of the blood-brain barrier (BBB) and its use, in particular to a nitric oxide donor that is controllable, A composition comprising a nitric oxide donor for improving the permeability of the blood-brain barrier, which allows the delivered nitric oxide to temporarily open the blood-brain barrier, thereby accumulating required substances in the brain, and uses thereof. Background technique [0002] The Blood-Brain Barrier is a defense system that exists in the living body and can prevent foreign substances such as bacteria or viruses flowing through the blood vessels from penetrating deep into the brain. The defense system as described above plays a very important role in protecting the brain, but at the same time, it has the problem of preventing the entry of artificially administered functional drugs into the brain. Although there is a method...
Claims
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IPC IPC(8): A61K31/655A61K31/095A61K38/06A61K31/136A61K31/04A61K31/295A61K31/5377A61K45/06A61P25/00A61P25/28A61P35/00A61P9/10A61K41/00A61K49/00A61K51/04A61K51/08
CPCA61K31/655A61K31/095A61K38/06A61K31/136A61K31/04A61K31/295A61K31/5377A61K45/06A61P25/00A61P25/28A61P35/00A61P9/10A61K49/0002A61K49/0052A61K51/04A61K41/00A61K51/0446A61K51/08A61K51/0463A61K31/40A61K2300/00A61K31/13A61K33/00A61K47/16A61K9/0085A61P43/00A61K49/006
Inventor 金园钟金泰廷
Owner POSTECH ACAD IND FOUND